Imodium (Loperamide HCl)

IMODIUMĀ®

Janssen-Ortho/ McNeil Consumer Products

Loperamide HCl

Antidiarrheal

Action And Clinical Pharmacology: Diarrhea may be defined as a failure or imbalance of one or a combination of activities in the gut which include secretion, absorption and motility. Loperamide has been shown to act on all of these functions via cholinergic, noncholinergic, opiate and nonopiate receptor-mediated mechanisms. In this way, loperamide effectively reduces fecal output and frequency, improves stool consistency and relieves symptoms of abdominal cramping and fecal incontinence.

Indications And Clinical Uses: As an adjunct to rehydration therapy for the symptomatic control of acute nonspecific diarrhea; for chronic diarrhea associated with inflammatory bowel disease; and for reducing the volume of discharge for ileostomies, colostomies and other intestinal resections.

Contra-Indications: Children under 2 years of age.

Known hypersensitivity to loperamide or any of the other components; cases in which constipation must be avoided.

Loperamide should not be used in the case of acute dysentery which is characterized by blood in stools and elevated temperature.

Loperamide must not be used in patients with acute ulcerative colitis and in pseudomembranous colitis associated with broad-spectrum antibiotics. In such patients, agents which inhibit intestinal motility or delay intestinal transit time have been reported to induce toxic megacolon. In general, loperamide should not be used when the inhibition of peristalsis is to be avoided. Discontinue loperamide therapy promptly if constipation, abdominal distention or ileus occurs or if other untoward symptoms develop.

Manufacturers’ Warnings In Clinical States: Children: The use of loperamide is not recommended for children under 12 years of age except on the advice of a physician (see Dosage).

Use loperamide with special caution in young children and those with compromised blood brain barrier (e.g., meningitis) because of the greater variability of response in these groups. Dehydration, particularly in young children, may further influence the variability of response to loperamide.

Since treatment of diarrhea with loperamide is only symptomatic, diarrhea should be treated causally whenever causal treatment is available. Fluid and electrolyte depletion may occur in patients who have diarrhea. The use of loperamide does not preclude the administration of appropriate fluid and electrolyte therapy.

Loperamide should be kept out of reach of children. Due to the particular ease with which the quick-dissolve tablets may be swallowed, special care should be taken when storing this product.

In case of accidental ingestion of loperamide by children, see Overdose.

Precautions: Pregnancy: Safe use of loperamide during pregnancy has not been established. Reproduction studies performed in the rat and the rabbit revealed no evidence of impaired fertility or harm to the fetus at dosage levels up to 30-fold the therapeutic dose for man. Therefore, loperamide should be used in pregnant women only when, in the opinion of the physician, the potential benefits outweigh the possible hazards.

Lactation: There is little information on the excretion of loperamide in human milk, but small amounts of the drug were detected in the milk of a nursing mother. Therefore, loperamide should not be administered to lactating women unless in the judgement of a physician, the potential benefits outweigh the possible risks.

Monitor patients with hepatic dysfunction for signs of CNS toxicity due to the extensive first pass metabolism of loperamide in the liver.

If improvement in symptoms of acute diarrhea is not observed within 48 hours, discontinue the use of loperamide and consult a physician.

Dependence Liability: Physical dependence to loperamide in humans has not been observed. However studies in morphine-dependent monkeys demonstrated that loperamide HCl at doses above those recommended for humans prevented signs of morphine withdrawal. However, in humans, the naloxone challenge pupil test, which when positive indicates opiate-like effects, performed after a single high dose, or after more than 2 years of therapeutic use of loperamide, was negative.

Adverse Reactions: The adverse effects reported in adults during clinical trials are difficult to distinguish from symptoms associated with the diarrheal syndrome. In adults, they were generally of a minor and self-limiting nature, e.g., abdominal pain or discomfort; drowsiness or dizziness; tiredness; dry mouth; nausea and vomiting; hypersensitivity, including skin rash. Constipation and/or abdominal distention have also been reported. In some very rare cases, particularly in which the treatment information had not been respected, these effects have been associated with ileus. Opiate-like effects (CNS) have been observed in young children (under 3 years of age).

Symptoms And Treatment Of Overdose: Symptoms: In case of overdosage (including relative overdosage due to hepatic dysfunction), CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia, respiratory depression) and ileus may occur. Children may be more sensitive to CNS effects than adults.

In clinical trials, an adult who took three 20 mg doses within a 24-hour period was nauseated after the second dose and vomited after the third dose. In studies designed to examine the potential for side effects, intentional ingestion of up to 60 mg of loperamide in a single dose to healthy subjects resulted in no significant adverse effects.

Treatment: Treatment is symptomatic and supportive. Appropriate standard methods of gastrointestinal decontamination may be employed. Activated charcoal administered promptly after ingestion of loperamide can reduce the amount of drug which is absorbed into the systemic circulation by as much as 9-fold.

In the event of overdosage, patients should be monitored for signs of CNS depression for at least 48 hours. If CNS depression is observed, naloxone may be useful. Since the duration of action of loperamide is longer than that of naloxone (which is 1 to 3 hours) repeated dosing with naloxone may be required. If responsive to naloxone, vital signs must be monitored carefully for recurrence of symptoms of drug overdose for at least 48 hours after the last dose of naloxone.

Since relatively little drug is excreted in the urine, forced diuresis is not expected to be effective for loperamide overdosage.

Physicians without experience in managing loperamide overdose should seek consultation with a Regional Poison Control Centre.

Dosage And Administration: Adults: Acute Diarrhea: 4 mg initially, followed by 2 mg after each unformed stool. Clinical studies indicate that diarrheal control may be achieved after the initial dose in 50% of patients. Daily dosage should not exceed 16 mg.

The quick-dissolve tablet is fast dissolving and can be taken without fluid. The tablet disintegrates within seconds on the surface of the tongue and is swallowed with the saliva.

Chronic Diarrhea: 4 mg initially, followed by 2 mg after each unformed stool until diarrhea is controlled; thereafter the dosage should be reduced to meet individual requirements. When the optimal daily dosage has thus been established, this amount can be administered as a single daily dose or in divided doses.

The average daily maintenance dosage used in clinical trials has been 4 to 8 mg. If improvement is not observed after treatment with 16 mg/day for 10 days, symptoms are unlikely to be controlled by further administration.

Children: Acute or Chronic Diarrhea: Loperamide should be used in children only on the advice of a physician. For children up to but not including 12 years of age, the following schedule will usually fulfill initial dosage requirements.

Following the first treatment day, it is recommended that subsequent doses (1 mg/10 kg body weight) be administered only after a loose stool and not exceed the maximum daily dose.

Duration of Treatment: Loperamide may be administered for prolonged periods of time. Blood, urine, liver and kidney function, ECG and ophthalmological examinations have revealed no significant abnormalities after several years of administration. No tolerance to the antidiarrheal effect has been observed. Naloxone pupil challenge studies in patients with chronic diarrhea who have received loperamide orally for prolonged periods indicate a lack of CNS effects.

Availability And Storage: Each light green elongated capsule shaped tablet contains: loperamide HCl 2 mg. Nonmedicinal ingredients: cellulose, colloidal silicon dioxide, D&C yellow No.10, dibasic calcium phosphate, FD&C blue No.1 and magnesium stearate. Bisulfites-, gluten-, lactose-, sodium- and tartrazine-free. Blister packs of 6, 12, 18 or 24 (supplied by McNeil Consumer Products). HDPE bottles of 100 and 500 (supplied by Janssen-Ortho). Store at room temperature, protect from light.

IMODIUMĀ® Janssen-Ortho/ McNeil Consumer Products Loperamide HCl Antidiarrheal

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